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Assay Detail

CHEMBL755332

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Compound was evaluated for functional potencies and efficacies at rat Nicotinic acetylcholine receptor alpha4-beta2
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 6 — Multiple protein complex / RNA
Curated By Autocuration

Target

Neuronal acetylcholine receptor; alpha4/beta2 (CHEMBL1907596)
Type PROTEIN COMPLEX
Organism Rattus norvegicus

Publication

Neuronal nicotinic acetylcholine receptors as targets for drug discovery.
Holladay MW, Dart MJ, Lynch JK.
J Med Chem (1997) 40 : 4169 -4194
PubMed 9435889 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 5 6.40 7.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL6623 EPIBATIDINE 1 7.80
CHEMBL335712 1 6.43
CHEMBL132966 RIVANICLINE 2.0 1 6.14
CHEMBL274525 ABT-418 1 5.22
CHEMBL667 ACETYLCHOLINE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL6623 EPIBATIDINE EC50 = 16.0 nM 7.80
CHEMBL335712 EC50 = 370.0 nM 6.43
CHEMBL132966 RIVANICLINE EC50 = 730.0 nM 6.14
CHEMBL274525 ABT-418 EC50 = 6000.0 nM 5.22
CHEMBL667 ACETYLCHOLINE EC50 = 270000.0 nM -